scholarly journals Antiproliferative Activity of Pt(IV) Conjugates Containing the Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) Ketoprofen and Naproxen †

2019 ◽  
Vol 20 (12) ◽  
pp. 3074 ◽  
Author(s):  
Mauro Ravera ◽  
Ilaria Zanellato ◽  
Elisabetta Gabano ◽  
Elena Perin ◽  
Beatrice Rangone ◽  
...  

Cisplatin and several non-steroidal anti-inflammatory drugs (NSAIDs) have been proven to act synergistically or at least additively on several tumor cell lines. Dual-action cisplatin-based Pt(IV) combos containing ketoprofen and naproxen offer good antiproliferative performance on a panel of human tumor cell lines, including a malignant pleural mesothelioma (MPM) one, a very chemoresistant tumor. The main reason of the increased activity relies on the enhanced lipophilicity of these Pt(IV) conjugates that in turn promotes increased cellular accumulation. A quick Pt(IV)→Pt(II) reduction generates the active cisplatin metabolite. The NSAID adjuvant action seems to be almost independent from cyclooxygenase-2 (COX-2) expression in the tumor cells under investigation (lung A-549, colon HT-29, HCT 116, SW480, ovarian A2780, and biphasic MPM MSTO-211H), but it seems to rely (at least in part) on the activation of the NSAID activated gene, NAG-1 (a member of the transforming growth factor beta, TGF-β, superfamily), which has been suggested to be involved in NSAID antiproliferative activity.

Biomolecules ◽  
2019 ◽  
Vol 9 (8) ◽  
pp. 315 ◽  
Author(s):  
Soraia I. Falcão ◽  
Ricardo C. Calhelha ◽  
Soumaya Touzani ◽  
Badiaâ Lyoussi ◽  
Isabel C. F. R. Ferreira ◽  
...  

Propolis is a resin manufactured by bees through the mixture of plant exudates and waxes with secreted substances from their metabolism, resulting in a complex mixture of natural substances of which quality depends on the phytogeographic and climatic conditions around the hive. The present study investigated the contribution of phenolic compounds to the cytotoxic and anti-inflammatory activities of propolis. The phenolic composition was evaluated by liquid chromatography with diode-array detection coupled to electrospray ionization tandem mass spectrometry (LC/DAD/ESI-MSn) analysis after phenolic extraction. The cytotoxicity of the extracts was checked using human tumor cell lines (MCF7- breast adenocarcinoma, NCI-H460- non-small cell lung carcinoma, HeLa- cervical carcinoma, HepG2- hepatocellular carcinoma, and MM127- malignant melanoma), as well as non-tumor cells (a porcine liver primary culture-PLP2). The anti-inflammatory activity was assessed using the murine macrophage (RAW 264.7) cell line. The results showed a composition rich in phenolic acids, such as caffeic and p-coumaric acid, as well as flavonoids, such as pinocembrin, pinobanksin, and pinobanksin-3-O-butyrate. Samples MP2 from Sefrou and MP3 from Moulay Yaâcoub presented a high concentration in phenolic compounds, while MP1 and MP4 from Boulemane and Immouzzer Mermoucha, respectively, showed similar composition with low bioactivity. The higher concentration of phenolic compound derivatives, which seems to be the most cytotoxic phenolic class, can explain the pronounced antitumor and anti-inflammatory activity observed for sample MP2.


Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 4005
Author(s):  
Simayijiang Aimaiti ◽  
Yohei Saito ◽  
Shuichi Fukuyoshi ◽  
Masuo Goto ◽  
Katsunori Miyake ◽  
...  

Seven new butanolides, peltanolides A–G (1–7), and two lignan glucosides, peltasides A (8) and B (9), along with eleven known compounds, 10–20, were isolated from a crude CH3OH/CH2Cl2 (1:1) extract of the fruit of Hernandia nymphaeifolia (Hernandiaceae). The structures of 1–9 were characterized by extensive 1D and 2D NMR spectroscopic and HRMS analysis. The absolute configurations of newly isolated compounds 1–9 were determined from data obtained by optical rotation and electronic circular dichroism (ECD) exciton chirality methods. Butanolides and lignan glucosides have not been isolated previously from this genus. Several isolated compounds were evaluated for antiproliferative activity against human tumor cell lines. Lignans 15 and 16 were slightly active against chemosensitive tumor cell lines A549 and MCF-7, respectively. Furthermore, both compounds displayed significant activity (IC50 = 5 µM) against a P-glycoprotein overexpressing multidrug-resistant tumor cell line (KB-VIN) but were less active against its parent chemosensitive cell line (KB).


Author(s):  
Karen Morales-Vela ◽  
Flor Celeste Pérez-Sánchez ◽  
Jose M. Padron ◽  
Olivia Márquez-Fernández

There are many species of endemic plants from Mexico, without food or commercial use, but with different applications in traditional medicine and valuable for their content of secondary metabolites. In this sense, we found two species of Cucurbitacea family plants natives of southeast and gulf of México, with traditionally use how soap and laundry agent, control of some pests, and it has also been used how infusion for the treatment of different types of dermatitis and stomachache. In the present work, we evaluate the antiproliferative activity in vitro, of six crude organic extracts, tested against six human tumor cell lines, A549 (lung), HBL-100 (breast), HeLa (cervix), SW1573 (lung), T-47D (breast) and WiDr (colon), the results indicated that at least three extracts from both species presents an interesting antiproliferative activity on five tumor cell lines.


2019 ◽  
Vol 19 (5) ◽  
pp. 424-436 ◽  
Author(s):  
Yulu Ma ◽  
Xi Zheng ◽  
Ping Zhu ◽  
Bei Liu ◽  
Hui Gao ◽  
...  

Introduction: Resveratrol and chalcones are lead compounds with good biological activities. </P><P> Method: In this study, a series of novel derivatives (6-38) between resveratrol and chalcone possessing piperazine moiety have been synthesized, and in vitro anti-inflammatory activity in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages and anti-proliferative effect on a panel of human tumor cell lines (Hela, A549 and SGC7901) by MTT assay were evaluated. </P><P> Result: The results demonstrated that the substituents of the NH group of piperazine ring had an obvious influence on biological activities. Especially, compounds 13, 17, 30, 31 and 36 showed good inhibitory effect on the generation of NO compared to dexamethasone. Furthermore, analogs 20, 21, 22 and 25 were found to be the better anti-proliferative effect on 3 human tumor cell lines, which were found to be a better cytotoxic activity to positive control 5-FU. Many compounds displayed low cytotoxic effect on normal cells L02. </P><P> Conclusion: Further FACs analysis showed that compounds 20 and 25 significantly induced apoptosis in A549 cell. These derivatives were considered as the potential anti-inflammatory and anti-tumor agents.


2012 ◽  
Vol 2012 ◽  
pp. 1-12 ◽  
Author(s):  
Lívia Câmara de Carvalho Galvão ◽  
Vivian Fernandes Furletti ◽  
Salete Meyre Fernandes Bersan ◽  
Marcos Guilherme da Cunha ◽  
Ana Lúcia Tasca Góis Ruiz ◽  
...  

This study aimed to evaluate the activity of essential oils (EOs) againstStreptococcus mutansbiofilm by chemically characterizing their fractions responsible for biological and antiproliferative activity. Twenty EO were obtained by hydrodistillation and submitted to the antimicrobial assay (minimum inhibitory (MIC) and bactericidal (MBC) concentrations) againstS. mutansUA159. Thin-layer chromatography and gas chromatography/mass spectrometry were used for phytochemical analyses. EOs were selected according to predetermined criteria and fractionated using dry column; the resulting fractions were assessed by MIC and MBC, selected as active fractions, and evaluated againstS. mutansbiofilm. Biofilms formed were examined using scanning electron microscopy. Selected EOs and their selected active fractions were evaluated for their antiproliferative activity against keratinocytes and seven human tumor cell lines. MIC and MBC values obtained for EO and their active fractions showed strong antimicrobial activity. Chemical analyses mainly showed the presence of terpenes. The selected active fractions inhibitedS. mutansbiofilm formation (P<0.05) did not affect glycolytic pH drop and were inactive against keratinocytes, normal cell line. In conclusion, EO showed activity at low concentrations, and their selected active fractions were also effective against biofilm formed byS. mutansand human tumor cell lines.


2005 ◽  
Vol 218 (2) ◽  
pp. 163-170 ◽  
Author(s):  
Sandra Huguenin ◽  
Francis Vacherot ◽  
Jocelyne Fleury-Feith ◽  
Jean-Pierre Riffaud ◽  
Dominique K. Chopin ◽  
...  

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